sodium independent organic anion transporters


Summary: A subclass of ORGANIC ANION TRANSPORTERS that do not rely directly or indirectly upon sodium ion gradients for the transport of organic ions.

Top Publications

  1. Monks N, Liu S, Xu Y, Yu H, Bendelow A, Moscow J. Potent cytotoxicity of the phosphatase inhibitor microcystin LR and microcystin analogues in OATP1B1- and OATP1B3-expressing HeLa cells. Mol Cancer Ther. 2007;6:587-98 pubmed
  2. Komatsu M, Furukawa T, Ikeda R, Takumi S, Nong Q, Aoyama K, et al. Involvement of mitogen-activated protein kinase signaling pathways in microcystin-LR-induced apoptosis after its selective uptake mediated by OATP1B1 and OATP1B3. Toxicol Sci. 2007;97:407-16 pubmed
  3. Gasser P, Orchinik M, Raju I, Lowry C. Distribution of organic cation transporter 3, a corticosterone-sensitive monoamine transporter, in the rat brain. J Comp Neurol. 2009;512:529-55 pubmed publisher
  4. Rodriguez Novoa S, Labarga P, Soriano V, Egan D, Albalater M, Morello J, et al. Predictors of kidney tubular dysfunction in HIV-infected patients treated with tenofovir: a pharmacogenetic study. Clin Infect Dis. 2009;48:e108-16 pubmed publisher
    ..This polymorphism may help to identify patients at greater risk for developing tenofovir-associated tubulopathy, and close monitoring of renal function is warranted for these patients. ..
  5. Enomoto A, Takeda M, Tojo A, Sekine T, Cha S, Khamdang S, et al. Role of organic anion transporters in the tubular transport of indoxyl sulfate and the induction of its nephrotoxicity. J Am Soc Nephrol. 2002;13:1711-20 pubmed
    ..These results suggest that rOAT1 and rOAT3 play an important role in the transcellular transport of IS and the induction of its nephrotoxicity. ..
  6. Cai H, Agrawal A, Putt D, Hashim M, Reddy A, Brodfuehrer J, et al. Assessment of the renal toxicity of novel anti-inflammatory compounds using cynomolgus monkey and human kidney cells. Toxicology. 2009;258:56-63 pubmed
    ..Thus, hOAT1 and/or hOAT3 may be responsible for the uptake of this series of drugs in renal PT cells, which may directly or indirectly lead to the observed nephrotoxicity in vivo. ..
  7. Hagenbuch N, Reichel C, Stieger B, Cattori V, Fattinger K, Landmann L, et al. Effect of phenobarbital on the expression of bile salt and organic anion transporters of rat liver. J Hepatol. 2001;34:881-7 pubmed
    ..The hepatic clearance of drugs and cholephilic organic anions is stimulated by phenobarbital (PB). Our aim was to analyze the effects of PB on the expression of hepatocellular bile salt and organic anion transporters...
  8. Itagaki S, Sugawara M, Kobayashi M, Nishimura S, Fujimoto M, Miyazaki K, et al. Major role of organic anion transporters in the uptake of phenolsulfonphthalein in the kidney. Eur J Pharmacol. 2003;475:85-92 pubmed
    ..We conclude that rOat1 and rOat3 are involved in the renal uptake of phenolsulfonphthalein and that phenolsulfonphthalein is a high-affinity substrate for rOat3 but is a relatively low-affinity substrate for rOat1. ..
  9. Sauvant C, Holzinger H, Gekle M. Prostaglandin E2 inhibits its own renal transport by downregulation of organic anion transporters rOAT1 and rOAT3. J Am Soc Nephrol. 2006;17:46-53 pubmed
    ..The described regulatory mechanism may also be of relevance in chronic inflammatory events. Moreover, the data presented could explain why increased plasma urate levels occur in diseases that go along with increased levels of PGE2. ..

More Information

Publications110 found, 100 shown here

  1. Nakayama H, Kitaichi K, Ito Y, Hashimoto K, Takagi K, Yokoi T, et al. The role of organic cation transporter-3 in methamphetamine disposition and its behavioral response in rats. Brain Res. 2007;1184:260-9 pubmed
    ..Thus, these results suggest that OCT3 may be a new molecular target to treat METH-related disorders such as drug abuse and schizophrenia. ..
  2. Chu X, Bleasby K, Yabut J, Cai X, Chan G, Hafey M, et al. Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein. J Pharmacol Exp Ther. 2007;321:673-83 pubmed
    ..However, the magnitude of interactions should be low, and the effects may not be clinically meaningful, due to the high safety margin of sitagliptin. ..
  3. Villar S, Brandoni A, Torres A. Time course of organic anion excretion in rats with bilateral ureteral obstruction: role of organic anion transporters (Oat1 and Oat3). Nephron Physiol. 2008;110:p45-56 pubmed publisher
    ..This study provides evidence regarding the importance of adjusting the dose regimens of negatively charged drugs during the different time phases of this pathology. ..
  4. Ueo H, Motohashi H, Katsura T, Inui K. Human organic anion transporter hOAT3 is a potent transporter of cephalosporin antibiotics, in comparison with hOAT1. Biochem Pharmacol. 2005;70:1104-13 pubmed
    ..In contrast, the uptake of these antibiotics by HEK-hOAT1 was within two-fold of that by control cells. In conclusion, hOAT3 plays a more important role than hOAT1 in the renal secretion of cephalosporin antibiotics. ..
  5. Ohtsuki S, Tomi M, Hata T, Nagai Y, Hori S, Mori S, et al. Dominant expression of androgen receptors and their functional regulation of organic anion transporter 3 in rat brain capillary endothelial cells; comparison of gene expression between the blood-brain and -retinal barriers. J Cell Physiol. 2005;204:896-900 pubmed
    ..The BBB function will be affected by the androgen levels in the brain and/or plasma via AR. ..
  6. Xiao Y, Nieves E, Angeletti R, Orr G, Wolkoff A. Rat organic anion transporting protein 1A1 (Oatp1a1): purification and phosphopeptide assignment. Biochemistry. 2006;45:3357-69 pubmed
    ..Whether phosphorylation near the C-terminus inhibits C-terminal oligomerization of oatp1a1, required for normal transport function, can be speculated upon but is as yet unknown. ..
  7. Whitley A, Sweet D, Walle T. Site-specific accumulation of the cancer preventive dietary polyphenol ellagic acid in epithelial cells of the aerodigestive tract. J Pharm Pharmacol. 2006;58:1201-9 pubmed
    ..Finally, Caco-2 cells were shown to express organic anion transporter 4 (OAT4) mRNA, as was the human large intestine. EA appears to be accumulated along the aerodigestive tract using OAT-like transporters, one of which might be OAT4. ..
  8. Mittur A, Wolkoff A, Kaplowitz N. The thiol sensitivity of glutathione transport in sidedness-sorted basolateral liver plasma membrane and in Oatp1-expressing HeLa cell membrane. Mol Pharmacol. 2002;61:425-35 pubmed
    ..These findings identify novel functional asymmetries in sinusoidal efflux and uptake of GSH and further clarify the role of Oatp1 in GSH transport. ..
  9. Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H. Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002;301:293-8 pubmed
  10. Kok T, Bloks V, Wolters H, Havinga R, Jansen P, Staels B, et al. Peroxisome proliferator-activated receptor alpha (PPARalpha)-mediated regulation of multidrug resistance 2 (Mdr2) expression and function in mice. Biochem J. 2003;369:539-47 pubmed
    ..The induction of Mdr2 mRNA and Mdr2 protein levels by fibrates is mediated by PPARalpha, while the induction of Mdr1a / 1b in vivo probably reflects a secondary phenomenon related to chronic PPARalpha activation...
  11. Okura T, Ito R, Ishiguro N, Tamai I, Deguchi Y. Blood-brain barrier transport of pramipexole, a dopamine D2 agonist. Life Sci. 2007;80:1564-71 pubmed
    ..These results suggest that pramipexole is, at least in part, transported across the BBB by an organic cation-sensitive transporter. The pramipexole transport in RBEC1 was pH-dependent, but sodium- and membrane potential-independent. ..
  12. Geier A, Dietrich C, Lammert F, Orth T, Mayet W, Matern S, et al. Regulation of organic anion transporters in a new rat model of acute and chronic cholangitis resembling human primary sclerosing cholangitis. J Hepatol. 2002;36:718-24 pubmed
    ..This might represent the first injury to hepatocytes in chronic cholangitis as an extension of liver injury from the level of cholangiocytes to hepatocytes in PSC. ..
  13. Jung D, Podvinec M, Meyer U, Mangelsdorf D, Fried M, Meier P, et al. Human organic anion transporting polypeptide 8 promoter is transactivated by the farnesoid X receptor/bile acid receptor. Gastroenterology. 2002;122:1954-66 pubmed
    ..OATP8 gene expression is regulated by bile acids via FXR/BAR. Induction of OATP8 could serve to maintain hepatic extraction of xenobiotics and peptides in conditions of increased intracellular bile acids. ..
  14. Alebouyeh M, Takeda M, Onozato M, Tojo A, Noshiro R, Hasannejad H, et al. Expression of human organic anion transporters in the choroid plexus and their interactions with neurotransmitter metabolites. J Pharmacol Sci. 2003;93:430-6 pubmed
    ..These results suggest that hOAT1 and hOAT3 are involved in the efflux of various neurotransmitter metabolites from the cerebrospinal fluid to the blood across the choroid plexus. ..
  15. van de Steeg E, Wagenaar E, van der Kruijssen C, Burggraaff J, de Waart D, Elferink R, et al. Organic anion transporting polypeptide 1a/1b-knockout mice provide insights into hepatic handling of bilirubin, bile acids, and drugs. J Clin Invest. 2010;120:2942-52 pubmed publisher
    ..Slco1a/1b-/- mice will provide excellent tools to study further the role of Oatp1a/1b transporters in physiology and drug disposition. ..
  16. Cha S, Sekine T, Fukushima J, Kanai Y, Kobayashi Y, Goya T, et al. Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001;59:1277-86 pubmed
    ..3 by fluorescent in situ hybridization analysis. These results suggest an important role of hOAT3 in the excretion/detoxification of endogenous and exogenous organic anions in the kidney. ..
  17. Tahara H, Shono M, Kusuhara H, Kinoshita H, Fuse E, Takadate A, et al. Molecular cloning and functional analyses of OAT1 and OAT3 from cynomolgus monkey kidney. Pharm Res. 2005;22:647-60 pubmed
    ..These results suggest that monkey is a good predictor of the renal uptake of organic anions in the human. ..
  18. Duan P, Li S, You G. Angiotensin II inhibits activity of human organic anion transporter 3 through activation of protein kinase Calpha: accelerating endocytosis of the transporter. Eur J Pharmacol. 2010;627:49-55 pubmed publisher
    ..We concluded that angiotensin II inhibited hOAT3 activity through the activation of PKCalpha, which led to an acceleration of hOAT3 endocytosis. ..
  19. Sakurai Y, Motohashi H, Ogasawara K, Terada T, Masuda S, Katsura T, et al. Pharmacokinetic significance of renal OAT3 (SLC22A8) for anionic drug elimination in patients with mesangial proliferative glomerulonephritis. Pharm Res. 2005;22:2016-22 pubmed
    ..These results suggest that the hOAT3 mRNA level is a significant marker of pharmacokinetics with which to predict the rate of elimination of cefazolin in patients with mesangial proliferative glomerulonephritis. ..
  20. Chen C, Cheng X, Dieter M, Tanaka Y, Klaassen C. Activation of cAMP-dependent signaling pathway induces mouse organic anion transporting polypeptide 2 expression. Mol Pharmacol. 2007;71:1159-64 pubmed
  21. Ugele B, Bahn A, Rex Haffner M. Functional differences in steroid sulfate uptake of organic anion transporter 4 (OAT4) and organic anion transporting polypeptide 2B1 (OATP2B1) in human placenta. J Steroid Biochem Mol Biol. 2008;111:1-6 pubmed publisher
    ..OATP2B1 seems not to be involved in de novo synthesis of placental estrogens but may contribute to the clearance of estrogen sulfates from foetal circulation. ..
  22. Han Y, Busler D, Hong Y, Tian Y, Chen C, Rodrigues A. Transporter studies with the 3-O-sulfate conjugate of 17alpha-ethinylestradiol: assessment of human kidney drug transporters. Drug Metab Dispos. 2010;38:1064-71 pubmed publisher
    ..6 microM; K(m2) = 195 microM). Based on the results of this study, we hypothesize that EE2-Sul is taken up into renal proximal tubule cells by OAT3, and OAT4 plays a role in its secretion into the renal brush border lumen. ..
  23. Klein K, Jüngst C, Mwinyi J, Stieger B, Krempler F, Patsch W, et al. The human organic anion transporter genes OAT5 and OAT7 are transactivated by hepatocyte nuclear factor-1? (HNF-1?). Mol Pharmacol. 2010;78:1079-87 pubmed publisher
    ..134, P < 0.05) or OAT7 (r = 0.461, P < 0.001) mRNA expression levels in surgical liver biopsies from 75 patients further supported an important role of HNF-1? in the regulation of OAT gene expression. ..
  24. Iida A, Saito S, Sekine A, Mishima C, Kondo K, Kitamura Y, et al. Catalog of 258 single-nucleotide polymorphisms (SNPs) in genes encoding three organic anion transporters, three organic anion-transporting polypeptides, and three NADH:ubiquinone oxidoreductase flavoproteins. J Hum Genet. 2001;46:668-83 pubmed
    ..These high-resolution maps will serve as a useful resource for analyzing potential associations between variations in these nine genes and differences in human susceptibilities to common diseases or response to drug therapies. ..
  25. Koh A, Simmons Willis T, Pritchard J, Grassl S, Ballatori N. Identification of a mechanism by which the methylmercury antidotes N-acetylcysteine and dimercaptopropanesulfonate enhance urinary metal excretion: transport by the renal organic anion transporter-1. Mol Pharmacol. 2002;62:921-6 pubmed
    ..This is the first molecular identification of a transport mechanism by which these antidotes may enhance urinary excretion of toxic metals. ..
  26. Jung K, Takeda M, Kim D, Tojo A, Narikawa S, Yoo B, et al. Characterization of ochratoxin A transport by human organic anion transporters. Life Sci. 2001;69:2123-35 pubmed
    ..These pharmacological characteristics of hOAT1 and hOAT3 may be significantly related with the events in the development of OTA-induced nephrotoxicity in the human kidney. ..
  27. Maeda A, Tsuruoka S, Kanai Y, Endou H, Saito K, Miyamoto E, et al. Evaluation of the interaction between nonsteroidal anti-inflammatory drugs and methotrexate using human organic anion transporter 3-transfected cells. Eur J Pharmacol. 2008;596:166-72 pubmed publisher
    ..The accumulation study using S2-hOAT3 cells might be useful for screening of potential interactions between methotrexate and new NSAIDs in vivo. ..
  28. De Zwart L, Scholten M, Monbaliu J, Annaert P, Van Houdt J, van den Wyngaert I, et al. The ontogeny of drug metabolizing enzymes and transporters in the rat. Reprod Toxicol. 2008;26:220-30 pubmed publisher
    ..Consideration of the ontogeny of metabolizing enzymes and transporters may improve the design and interpretation of results of toxicity studies in juvenile animals...
  29. Miao Z, Yan S, Wang J, Wang B, Li Y, Xing X, et al. Insulin resistance acts as an independent risk factor exacerbating high-purine diet induced renal injury and knee joint gouty lesions. Inflamm Res. 2009;58:659-68 pubmed publisher
    ..Our data demonstrated strong evidence indicating that insulin resistance acts as an independent risk factor predisposing OLETF rats more susceptible to the development of hyperuricemia and gouty arthritis following high-purine load. ..
  30. Poirier A, Cascais A, Funk C, Lave T. Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn. 2009;36:585-611 pubmed publisher
    ..More data are needed to support more general applications of the proposed approach including its use for metabolized compounds. ..
  31. Eraly S, Hamilton B, Nigam S. Organic anion and cation transporters occur in pairs of similar and similarly expressed genes. Biochem Biophys Res Commun. 2003;300:333-42 pubmed
    ..Finally, we find that pair-members have similar tissue distributions, suggesting that the pairing might exist to facilitate the co-regulation of the genes within each pair. ..
  32. Liu Y, Binz J, Numerick M, Dennis S, Luo G, Desai B, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003;112:1678-87 pubmed
    ..The hepatoprotection seen in these animal models by the synthetic FXR agonist suggests FXR agonists may be useful in the treatment of cholestatic liver disease...
  33. Koitabashi Y, Kumai T, Matsumoto N, Watanabe M, Sekine S, Yanagida Y, et al. Orange juice increased the bioavailability of pravastatin, 3-hydroxy-3-methylglutaryl CoA reductase inhibitor, in rats and healthy human subjects. Life Sci. 2006;78:2852-9 pubmed
    ..In conclusion, orange juice increases the bioavailability of pravastatin administered orally. Oatp1 and oatp2 may be related to increases of pharmacokinetics of pravastatin by orange juice...
  34. Matsuzaki T, Watanabe H, Yoshitome K, Morisaki T, Hamada A, Nonoguchi H, et al. Downregulation of organic anion transporters in rat kidney under ischemia/reperfusion-induced acute [corrected] renal failure. Kidney Int. 2007;71:539-47 pubmed
    ..Cobalt treatment has a significant protective effect on ischemia-induced ARF, being accompanied by the restoration of rOAT3 and/or Na(+)/K(+)-ATPase function. ..
  35. Evers R, Chu X. Role of the murine organic anion-transporting polypeptide 1b2 (Oatp1b2) in drug disposition and hepatotoxicity. Mol Pharmacol. 2008;74:309-11 pubmed publisher
    ..Taken together, these data illustrate that Oatp1b2(-/-) mice are an important new model to investigate the role of this transporter in drug disposition and hepatotoxicity. ..
  36. Li B, Li L, Donaldson P, Lim J. Dynamic regulation of GSH synthesis and uptake pathways in the rat lens epithelium. Exp Eye Res. 2010;90:300-7 pubmed publisher
    ..Finally, we also describe the identification of a putative GSH transporter which is most likely to mediate GSH uptake in this region...
  37. Gibbs J, Thomas S. The distribution of the anti-HIV drug, 2'3'-dideoxycytidine (ddC), across the blood-brain and blood-cerebrospinal fluid barriers and the influence of organic anion transport inhibitors. J Neurochem. 2002;80:392-404 pubmed
    ..AZT did not effect the accumulation of [3H]ddC, indicating that when these nucleoside analogues are used in anti-HIV combination therapy, the CNS distribution of ddC is unchanged. ..
  38. Lim S, Im Y, Bae C, Han S, Kim S, Han H. Protective effect of morin on the imipenem-induced nephrotoxicity in rabbits. Arch Pharm Res. 2008;31:1060-5 pubmed publisher
    ..In conclusion, the present study suggests that morin might be beneficial to reduce the nephrotoxicity of imipenem, at least in part, via the inhibition of OAT3-mediated renal excretion of imipenem. ..
  39. van de Steeg E, van der Kruijssen C, Wagenaar E, Burggraaff J, Mesman E, Kenworthy K, et al. Methotrexate pharmacokinetics in transgenic mice with liver-specific expression of human organic anion-transporting polypeptide 1B1 (SLCO1B1). Drug Metab Dispos. 2009;37:277-81 pubmed publisher
    ..SLCO1B1 transgenic mice could be a useful tool in studying the in vivo role of human OATP1B1 in drug pharmacokinetics. ..
  40. Maeda A, Tsuruoka S, Ushijima K, Kanai Y, Endou H, Saito K, et al. Drug interaction between celecoxib and methotrexate in organic anion transporter 3-transfected renal cells and in rats in vivo. Eur J Pharmacol. 2010;640:168-71 pubmed publisher
  41. Shima J, Komori T, Taylor T, Stryke D, Kawamoto M, Johns S, et al. Genetic variants of human organic anion transporter 4 demonstrate altered transport of endogenous substrates. Am J Physiol Renal Physiol. 2010;299:F767-75 pubmed publisher
  42. Brady K, Dushkin H, Förnzler D, Koike T, Magner F, Her H, et al. A novel putative transporter maps to the osteosclerosis (oc) mutation and is not expressed in the oc mutant mouse. Genomics. 1999;56:254-61 pubmed
    ..In situ studies show that Roct is expressed in developing bone. We propose that the absence of Roct expression results in an osteopetrosis phenotype in mice. ..
  43. Kojima R, Sekine T, Kawachi M, Cha S, Suzuki Y, Endou H. Immunolocalization of multispecific organic anion transporters, OAT1, OAT2, and OAT3, in rat kidney. J Am Soc Nephrol. 2002;13:848-57 pubmed
    ..These results on the distribution of each OAT isoform will facilitate the understanding of the role of OATs in the renal processing of organic anions. ..
  44. Zhou F, Pan Z, Ma J, You G. Mutational analysis of histidine residues in human organic anion transporter 4 (hOAT4). Biochem J. 2004;384:87-92 pubmed
    ..Therefore modification of His-469 is responsible for the inhibition of hOAT4 by DEPC. ..
  45. Wood C, Cousins R, Zhang D, Keller Wood M. Ontogeny of expression of organic anion transporters 1 and 3 in ovine fetal and neonatal kidney. Exp Biol Med (Maywood). 2005;230:668-73 pubmed
  46. Taft D, Dontabhaktuni A, Babayeva M, Nakatani Freshwater T, Savant I. Application of the isolated perfused rat kidney model to assess gender effects on drug excretion. Drug Dev Ind Pharm. 2006;32:919-28 pubmed
    ..The renal excretion of organic anions is reduced in female rats, possibly due to gender differences in expression and/or activity of membrane transporters (both basolateral and luminal) in the kidney. ..
  47. Hawkins B, Ocheltree S, Norwood K, Egleton R. Decreased blood-brain barrier permeability to fluorescein in streptozotocin-treated rats. Neurosci Lett. 2007;411:1-5 pubmed
    ..These data indicate that diabetes may lead to changes in efflux transporters at the BBB and have implications for delivery of therapeutics to the central nervous system. ..
  48. Nilwarangkoon S, Anzai N, Shiraya K, Yu E, Islam R, Cha S, et al. Role of mouse organic anion transporter 3 (mOat3) as a basolateral prostaglandin E2 transport pathway. J Pharmacol Sci. 2007;103:48-55 pubmed
  49. Fujimoto Y, Kitaichi K, Nakayama H, Ito Y, Takagi K, Takagi K, et al. The pharmacokinetic properties of methamphetamine in rats with previous repeated exposure to methamphetamine: the differences between Long-Evans and Wistar rats. Exp Anim. 2007;56:119-29 pubmed
  50. Cihlar T, Ray A, Laflamme G, Vela J, Tong L, Fuller M, et al. Molecular assessment of the potential for renal drug interactions between tenofovir and HIV protease inhibitors. Antivir Ther. 2007;12:267-72 pubmed
    ..These data indicate a low potential of PIs to interfere with the active tubular secretion of TFV and to alter the clinical renal safety profile of TDF. ..
  51. Sato M, Iwanaga T, Mamada H, Ogihara T, Yabuuchi H, Maeda T, et al. Involvement of uric acid transporters in alteration of serum uric acid level by angiotensin II receptor blockers. Pharm Res. 2008;25:639-46 pubmed
    ..Furthermore losartan could inhibit ATP-dependent uric acid secretion by MRP4. These effects may explain partially the alteration of serum uric acid level by ARBs. ..
  52. Meng L, Wang P, Wolkoff A, Kim R, Tirona R, Hofmann A, et al. Transport of the sulfated, amidated bile acid, sulfolithocholyltaurine, into rat hepatocytes is mediated by Oatp1 and Oatp2. Hepatology. 2002;35:1031-40 pubmed
  53. Shitara Y, Itoh T, Sato H, Li A, Sugiyama Y. Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. J Pharmacol Exp Ther. 2003;304:610-6 pubmed
    ..From these results, we conclude that the DDI between CER and CsA is mainly due to the inhibition of transporter (at least partly OATP2)-mediated uptake in the liver. ..
  54. Sykes D, Sweet D, Lowes S, Nigam S, Pritchard J, Miller D. Organic anion transport in choroid plexus from wild-type and organic anion transporter 3 (Slc22a8)-null mice. Am J Physiol Renal Physiol. 2004;286:F972-8 pubmed
  55. Kitaichi K, Fukuda M, Nakayama H, Aoyama N, Ito Y, Fujimoto Y, et al. Behavioral changes following antisense oligonucleotide-induced reduction of organic cation transporter-3 in mice. Neurosci Lett. 2005;382:195-200 pubmed
    ..c.), but did not affect spontaneous locomotor activity. These results suggest that OCT3 might become a novel molecular target to treat depression and other diseases related to monoaminergic neuronal systems. ..
  56. Erdman A, Mangravite L, Urban T, Lagpacan L, Castro R, De La Cruz M, et al. The human organic anion transporter 3 (OAT3; SLC22A8): genetic variation and functional genomics. Am J Physiol Renal Physiol. 2006;290:F905-12 pubmed
    ..This variant exhibited a reduced ability to transport ES, but a preserved ability to transport CIM. These data suggest that genetic variation in OAT3 may contribute to variation in the disposition of drugs. ..
  57. Ishiguro N, Maeda K, Kishimoto W, Saito A, Harada A, Ebner T, et al. Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos. 2006;34:1109-15 pubmed
    ..These results suggest that OATP1B3 is predominantly involved in the hepatic uptake of telmisartan in humans. ..
  58. Dietrich C, Martin I, Porn A, Voigt S, Gartung C, Trautwein C, et al. Fasting induces basolateral uptake transporters of the SLC family in the liver via HNF4alpha and PGC1alpha. Am J Physiol Gastrointest Liver Physiol. 2007;293:G585-90 pubmed
    ..We conclude that upregulation of the basolateral bile acid transporters Ntcp, Oatp1, and Oatp2 in fasted rats is mediated via the HNF4alpha/PGC-1alpha pathway. ..
  59. Tang W, Stearns R, Chen Q, Bleasby K, Teffera Y, Colletti A, et al. Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats. Xenobiotica. 2008;38:223-37 pubmed
    ..This case study demonstrates that an integrated strategy, incorporating both rapid screening and mechanistic investigations, is of particular value in supporting drug discovery efforts and decision-making processes. ..
  60. Chen J, Terada T, Ogasawara K, Katsura T, Inui K. Adaptive responses of renal organic anion transporter 3 (OAT3) during cholestasis. Am J Physiol Renal Physiol. 2008;295:F247-52 pubmed publisher
    ..In conclusion, the present study clearly demonstrated that OAT3 is responsible for renal secretion of bile acids during cholestasis and that the pharmacokinetic profile of OAT3 substrates may be affected by cholestasis. ..
  61. Hamada A, Sissung T, Price D, Danesi R, Chau C, Sharifi N, et al. Effect of SLCO1B3 haplotype on testosterone transport and clinical outcome in caucasian patients with androgen-independent prostatic cancer. Clin Cancer Res. 2008;14:3312-8 pubmed publisher
    ..023) than patients carrying TT/AA and TG/GA haplotypes. The common SLCO1B3 GG/AA haplotype is associated with impaired testosterone transport and improved survival in patients with prostatic cancer. ..
  62. Morisaki T, Matsuzaki T, Yokoo K, Kusumoto M, Iwata K, Hamada A, et al. Regulation of renal organic ion transporters in cisplatin-induced acute kidney injury and uremia in rats. Pharm Res. 2008;25:2526-33 pubmed publisher
    ..IS could be involved in the mechanism of down-regulation of rOAT1, rOAT3 and rMATE1 under cisplatin-induced AKI. ..
  63. Minuesa G, Volk C, Molina Arcas M, Gorboulev V, Erkizia I, Arndt P, et al. Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3. J Pharmacol Exp Ther. 2009;329:252-61 pubmed publisher
    ..Finally, 3TC is a novel substrate for hOCTs and the inhibition of its uptake at low concentrations of ABC and AZT could have implications for the pharmacokinetics of 3TC. ..
  64. Amphoux A, Millan M, Cordi A, Bonisch H, Vialou V, Mannoury La Cour C, et al. Inhibitory and facilitory actions of isocyanine derivatives at human and rat organic cation transporters 1, 2 and 3: a comparison to human alpha 1- and alpha 2-adrenoceptor subtypes. Eur J Pharmacol. 2010;634:1-9 pubmed publisher
  65. Li S, Duan P, You G. Regulation of human organic anion transporter 3 by peptide hormone bradykinin. J Pharmacol Exp Ther. 2010;333:970-5 pubmed publisher
  66. Bednarczyk D. Fluorescence-based assays for the assessment of drug interaction with the human transporters OATP1B1 and OATP1B3. Anal Biochem. 2010;405:50-8 pubmed publisher
    ..The in vitro fluorescence-based assays described here using 8-FcA as the substrate are convenient and rapid and have utility in screening drug candidates for potential drug-drug interactions with OATP1B1 and OATP1B3. ..
  67. Deguchi T, Ohtsuki S, Otagiri M, Takanaga H, Asaba H, Mori S, et al. Major role of organic anion transporter 3 in the transport of indoxyl sulfate in the kidney. Kidney Int. 2002;61:1760-8 pubmed
    ..Mutual inhibition of these uremic toxins via OAT3 may accelerate their accumulation in the body and, thereby, the progression of nephrotoxicity in uremia. ..
  68. Ohtsuki S, Asaba H, Takanaga H, Deguchi T, Hosoya K, Otagiri M, et al. Role of blood-brain barrier organic anion transporter 3 (OAT3) in the efflux of indoxyl sulfate, a uremic toxin: its involvement in neurotransmitter metabolite clearance from the brain. J Neurochem. 2002;83:57-66 pubmed
    ..Therefore, inhibition of the brain-to-blood transport involving OAT3 would occur in uremia and lead to the accumulation of neurotransmitter metabolites and drugs in the brain...
  69. Mori S, Takanaga H, Ohtsuki S, Deguchi T, Kang Y, Hosoya K, et al. Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells. J Cereb Blood Flow Metab. 2003;23:432-40 pubmed
    ..This HVA efflux transport system is likely to play an important role in controlling the level of HVA in the CNS. ..
  70. Rost D, Herrmann T, Sauer P, Schmidts H, Stieger B, Meier P, et al. Regulation of rat organic anion transporters in bile salt-induced cholestatic hepatitis: effect of ursodeoxycholate. Hepatology. 2003;38:187-95 pubmed
    ..In conclusion, we show that CA feeding may cause cholestasis associated with a posttranscriptional down-regulation of Oatp4. UDCA may prevent impairment of hepatic function by restoring hepatic transporter expression. ..
  71. Lungkaphin A, Lewchalermwongse B, Chatsudthipong V. Relative contribution of OAT1 and OAT3 transport activities in isolated perfused rabbit renal proximal tubules. Biochim Biophys Acta. 2006;1758:789-95 pubmed
    ..The relative contribution of both transporters depends on their relative expression levels and may possibly be affected by the activity of NaDC3 in RPT. ..
  72. Brandoni A, Anzai N, Kanai Y, Endou H, Torres A. Renal elimination of p-aminohippurate (PAH) in response to three days of biliary obstruction in the rat. The role of OAT1 and OAT3. Biochim Biophys Acta. 2006;1762:673-82 pubmed
    ..The present study demonstrates the key role of OAT1 expression in the impaired elimination of PAH after 3 days of obstructive cholestasis. ..
  73. Briz O, Romero M, Martinez Becerra P, Macias R, Perez M, Jimenez F, et al. OATP8/1B3-mediated cotransport of bile acids and glutathione: an export pathway for organic anions from hepatocytes?. J Biol Chem. 2006;281:30326-35 pubmed
  74. Vicens M, Medarde M, Macias R, Larena M, Villafaina A, Serrano M, et al. Novel cationic and neutral glycocholic acid and polyamine conjugates able to inhibit transporters involved in hepatic and intestinal bile acid uptake. Bioorg Med Chem. 2007;15:2359-67 pubmed
  75. Fujiyama N, Shitara Y, Ito K, Masubuchi Y, Horie T. Down-regulation of hepatic transporters for BSP in rats with indomethacin-induced intestinal injury. Biol Pharm Bull. 2007;30:556-61 pubmed
  76. Umehara K, Iwatsubo T, Noguchi K, Kamimura H. Functional involvement of organic cation transporter1 (OCT1/Oct1) in the hepatic uptake of organic cations in humans and rats. Xenobiotica. 2007;37:818-31 pubmed
  77. Abe M, Toyohara T, Ishii A, Suzuki T, Noguchi N, Akiyama Y, et al. The HMG-CoA reductase inhibitor pravastatin stimulates insulin secretion through organic anion transporter polypeptides. Drug Metab Pharmacokinet. 2010;25:274-82 pubmed
    ..In addition, insulin secretion from isolated islets was enhanced by pravastatin. These data suggest that pravastatin has pleiotropic effects on islets through membrane transport under high fat/glucose conditions. ..
  78. Reichel V, Kläs J, Fricker G, Masereeuw R. Fluo-cAMP is transported by multidrug resistance-associated protein isoform 4 in rat choroid plexus. J Neurochem. 2010;115:200-8 pubmed publisher
    ..Therefore, fluo-cAMP can be used as fluorescent model compound for studying involvement of Mrp4 in signalling pathways and neuroprotection in CP. ..
  79. Simonson G, Vincent A, Roberg K, Huang Y, Iwanij V. Molecular cloning and characterization of a novel liver-specific transport protein. J Cell Sci. 1994;107 ( Pt 4):1065-72 pubmed
    ..Overall, we have cloned a novel transporter that is preferentially expressed in liver, is located on the sinusoidal domain of the plasma membrane and represents a marker for the late stage of liver development. ..
  80. Takeda M, Babu E, Narikawa S, Endou H. Interaction of human organic anion transporters with various cephalosporin antibiotics. Eur J Pharmacol. 2002;438:137-42 pubmed
  81. Sweet D, Miller D, Pritchard J, Fujiwara Y, Beier D, Nigam S. Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem. 2002;277:26934-43 pubmed
    ..These data indicate a key role for Oat3 in systemic detoxification and in control of the organic anion distribution in cerebrospinal fluid. ..
  82. Geier A, Kim S, Gerloff T, Dietrich C, Lammert F, Karpen S, et al. Hepatobiliary organic anion transporters are differentially regulated in acute toxic liver injury induced by carbon tetrachloride. J Hepatol. 2002;37:198-205 pubmed
    ..Maintained binding activity of RXRalpha:RARalpha may explain differences in Mrp2 expression. ..
  83. Deguchi T, Kusuhara H, Takadate A, Endou H, Otagiri M, Sugiyama Y. Characterization of uremic toxin transport by organic anion transporters in the kidney. Kidney Int. 2004;65:162-74 pubmed
    ..Both OAT1 and OAT3 contribute almost equally to the renal uptake of IS. OAT3 mainly accounts for CMPF uptake by the kidney, while OAT1 mainly accounts for IA and HA uptake. ..
  84. Meier Abt F, Faulstich H, Hagenbuch B. Identification of phalloidin uptake systems of rat and human liver. Biochim Biophys Acta. 2004;1664:64-9 pubmed
    ..Therefore, we conclude that rat Oatp1b2 as well as human OATP1B1 and OATP1B3 are responsible for phalloidin uptake into rat and human hepatocytes. ..
  85. Sasaki M, Suzuki H, Aoki J, Ito K, Meier P, Sugiyama Y. Prediction of in vivo biliary clearance from the in vitro transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II monolayer expressing both rat organic anion transporting polypeptide 4 and multidrug resistan. Mol Pharmacol. 2004;66:450-9 pubmed
    ..The double-transfected MDCK II monolayer may be useful in analyzing the hepatic vectorial transport of organic anions and in predicting in vivo biliary clearance. ..
  86. Popowski K, Eloranta J, Saborowski M, Fried M, Meier P, Kullak Ublick G. The human organic anion transporter 2 gene is transactivated by hepatocyte nuclear factor-4 alpha and suppressed by bile acids. Mol Pharmacol. 2005;67:1629-38 pubmed
    ..Hepatic uptake of hOAT2 substrates may thus be decreased in disease conditions associated with elevated intracellular levels of bile acids. ..
  87. Niemi M, Kivistö K, Hofmann U, Schwab M, Eichelbaum M, Fromm M. Fexofenadine pharmacokinetics are associated with a polymorphism of the SLCO1B1 gene (encoding OATP1B1). Br J Clin Pharmacol. 2005;59:602-4 pubmed
  88. Lowes S, Sykes D, Breen C, Ragone L, Miller D. Multiple components of 2,4-dichlorophenoxyacetic acid uptake by rat choroid plexus. J Pharmacol Exp Ther. 2005;315:136-43 pubmed
    ..Thus, the first step in transport of 2,4-D from cerebrospinal fluid to blood involves two transporters: Oat3 and a PAH-insensitive, sodium-independent transporter. Based on inhibitor profile, the latter may be Oatp3. ..
  89. Donner M, Schumacher S, Warskulat U, Heinemann J, Haussinger D. Obstructive cholestasis induces TNF-alpha- and IL-1 -mediated periportal downregulation of Bsep and zonal regulation of Ntcp, Oatp1a4, and Oatp1b2. Am J Physiol Gastrointest Liver Physiol. 2007;293:G1134-46 pubmed
    ..Periportal downregulation of Ntcp and induction of Oatp1a4 and Oatp1b2 may represent adaptive mechanisms to reduce cholestatic injury in hepatocytes with profound downregulation of Bsep and Mrp2...
  90. Wang P, Hata S, Xiao Y, Murray J, Wolkoff A. Topological assessment of oatp1a1: a 12-transmembrane domain integral membrane protein with three N-linked carbohydrate chains. Am J Physiol Gastrointest Liver Physiol. 2008;294:G1052-9 pubmed publisher
    ..This was in accord with the finding that fully unglycosylated oatp1a1 was well expressed but located intracellularly with limited transport ability as a consequence of its reduced cell surface expression. ..
  91. Hagos Y, Krick W, Braulke T, Mühlhausen C, Burckhardt G, Burckhardt B. Organic anion transporters OAT1 and OAT4 mediate the high affinity transport of glutarate derivatives accumulating in patients with glutaric acidurias. Pflugers Arch. 2008;457:223-31 pubmed publisher
  92. Rödiger M, Zhang X, Ugele B, Gersdorff N, Wright S, Burckhardt G, et al. Organic anion transporter 3 (OAT3) and renal transport of the metal chelator 2,3-dimercapto-1-propanesulfonic acid (DMPS). Can J Physiol Pharmacol. 2010;88:141-6 pubmed publisher
    ..On the basis of the substantial interaction of OAT3 with DMPSS, we conclude that OAT3 represents the dominant basolateral player in renal detoxification processes resulting from use of DMPS. ..